6TPG
 
 | | Crystal structure of the Orexin-2 receptor in complex with EMPA at 2.74 A resolution | | Descriptor: | N-ethyl-2-[(6-methoxypyridin-3-yl)-(2-methylphenyl)sulfonyl-amino]-N-(pyridin-3-ylmethyl)ethanamide, OLEIC ACID, Orexin receptor type 2,GlgA glycogen synthase,Hypocretin receptor-2, ... | | Authors: | Rappas, M, Ali, A, Bennett, K.A, Brown, J.D, Bucknell, S.J, Congreve, M, Cooke, R.M, Cseke, G, de Graaf, C, Dore, A.S, Errey, J.C, Jazayeri, A, Marshall, F.H, Mason, J.S, Mould, R, Patel, J.C, Tehan, B.G, Weir, M, Christopher, J.A. | | Deposit date: | 2019-12-13 | | Release date: | 2020-01-01 | | Last modified: | 2024-01-24 | | Method: | X-RAY DIFFRACTION (2.741 Å) | | Cite: | Comparison of Orexin 1 and Orexin 2 Ligand Binding Modes Using X-ray Crystallography and Computational Analysis.
J.Med.Chem., 63, 2020
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9LRE
 | | Cryo-EM structure of the histamine H4 receptor-Gi protein complex (Overall) | | Descriptor: | Guanine nucleotide-binding protein G(I)/G(S)/G(O) subunit gamma-2, Guanine nucleotide-binding protein G(I)/G(S)/G(T) subunit beta-1, Guanine nucleotide-binding protein G(i) subunit alpha-1, ... | | Authors: | Matsuzaki, Y, Sano, F.K, Oshima, H.S, Akasaka, H, Kobayashi, K, Tanaka, T, Itoh, Y, Shihoya, W, Kise, Y, Kusakizako, T, Nureki, O. | | Deposit date: | 2025-01-30 | | Release date: | 2025-06-11 | | Method: | ELECTRON MICROSCOPY (2.84 Å) | | Cite: | Structural insights into ligand recognition and G protein preferences across histamine receptor
To Be Published
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9LYD
 | | Cryo-EM structure of GPR3-1IU9 complex | | Descriptor: | G-protein coupled receptor 3,Aspartate racemase | | Authors: | Hua, T, Liu, Z.J, Li, X.T, Chang, H. | | Deposit date: | 2025-02-19 | | Release date: | 2025-04-09 | | Last modified: | 2025-04-16 | | Method: | ELECTRON MICROSCOPY (3.66 Å) | | Cite: | Structural basis of oligomerization-modulated activation and autoinhibition of orphan receptor GPR3.
Cell Rep, 44, 2025
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9LRB
 | | Cryo-EM structure of the histamine H1 receptor-Gs protein complex | | Descriptor: | Guanine nucleotide-binding protein G(I)/G(S)/G(O) subunit gamma-2, Guanine nucleotide-binding protein G(I)/G(S)/G(T) subunit beta-1, Guanine nucleotide-binding protein G(s) subunit alpha isoforms short, ... | | Authors: | Matsuzaki, Y, Sano, F.K, Oshima, H.S, Akasaka, H, Kobayashi, K, Tanaka, T, Itoh, Y, Shihoya, W, Kise, Y, Kusakizako, T, Nureki, O. | | Deposit date: | 2025-01-30 | | Release date: | 2025-06-11 | | Method: | ELECTRON MICROSCOPY (2.77 Å) | | Cite: | Structural insights into ligand recognition and G protein preferences across histamine receptors
To Be Published
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9LRD
 | | Cryo-EM structure of the histamine H1 receptor-Gi protein complex | | Descriptor: | Guanine nucleotide-binding protein G(I)/G(S)/G(O) subunit gamma-2, Guanine nucleotide-binding protein G(I)/G(S)/G(T) subunit beta-1, Guanine nucleotide-binding protein G(i) subunit alpha-1, ... | | Authors: | Matsuzaki, Y, Sano, F.K, Oshima, H.S, Akasaka, H, Kobayashi, K, Tanaka, T, Itoh, Y, Shihoya, W, Kise, Y, Kusakizako, T, Nureki, O. | | Deposit date: | 2025-01-30 | | Release date: | 2025-06-11 | | Last modified: | 2025-06-18 | | Method: | ELECTRON MICROSCOPY (3.23 Å) | | Cite: | Structural insights into ligand recognition and G protein preferences across histamine receptors
To Be Published
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9LMP
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9LGM
 | | Cryo-EM structure of GPR4 complexed with Gs in pH8.0 | | Descriptor: | G-protein coupled receptor 4, Guanine nucleotide-binding protein G(I)/G(S)/G(O) subunit gamma-2, Guanine nucleotide-binding protein G(I)/G(S)/G(T) subunit beta-1, ... | | Authors: | Yue, X.L, Wu, L.J, Hua, T, Liu, Z.J. | | Deposit date: | 2025-01-10 | | Release date: | 2025-04-23 | | Last modified: | 2025-06-25 | | Method: | ELECTRON MICROSCOPY (2.84 Å) | | Cite: | Structural basis of stepwise proton sensing-mediated GPCR activation.
Cell Res., 35, 2025
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9LYB
 | | Cryo-EM structure of GPR3-G protein-monomer complex | | Descriptor: | G-protein coupled receptor 3, Guanine nucleotide-binding protein G(I)/G(S)/G(O) subunit gamma-2, Guanine nucleotide-binding protein G(I)/G(S)/G(T) subunit beta-1, ... | | Authors: | Hua, T, Liu, Z.J, Li, X.T, Chang, H. | | Deposit date: | 2025-02-19 | | Release date: | 2025-04-09 | | Last modified: | 2025-04-16 | | Method: | ELECTRON MICROSCOPY (3.16 Å) | | Cite: | Structural basis of oligomerization-modulated activation and autoinhibition of orphan receptor GPR3.
Cell Rep, 44, 2025
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9UY3
 | | Anamorelin bound growth hormone secretagogue receptor in complex with Gq | | Descriptor: | 2-azanyl-N-[(2R)-1-[(3S)-3-[dimethylamino(methyl)carbamoyl]-3-(phenylmethyl)piperidin-1-yl]-3-(1H-indol-3-yl)-1-oxidanylidene-propan-2-yl]-2-methyl-propanamide, CHOLESTEROL, Engineered G-alpha-q subunit, ... | | Authors: | Wang, R, Sun, J, Liu, H, Guo, S, Zhang, Y, Hu, W, Wang, J, Liu, H, Zhuang, Y, Jiang, Y, Xie, X, Xu, H.E, Wang, Y. | | Deposit date: | 2025-05-14 | | Release date: | 2025-07-02 | | Method: | ELECTRON MICROSCOPY (2.52 Å) | | Cite: | Molecular recognition of two approved drugs Macimorelin and Anamorelin by the growth hormone secretagogue receptor.
Acta Pharmacol.Sin., 2025
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9V2N
 | | Macimorelin bound growth hormone secretagogue receptor in complex with Gq | | Descriptor: | Engineered G-alpha-q subunit, Guanine nucleotide-binding protein G(I)/G(S)/G(O) subunit gamma-2, Guanine nucleotide-binding protein G(I)/G(S)/G(T) subunit beta-1, ... | | Authors: | Wang, R, Sun, J, Liu, H, Guo, S, Zhang, Y, Hu, W, Wang, J, Liu, H, Zhuang, Y, Jiang, Y, Xie, X, Xu, H, Wang, Y. | | Deposit date: | 2025-05-20 | | Release date: | 2025-07-02 | | Method: | ELECTRON MICROSCOPY (2.63 Å) | | Cite: | Molecular recognition of two approved drugs Macimorelin and Anamorelin by the growth hormone secretagogue receptor.
Acta Pharmacol.Sin., 2025
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9M1H
 | | Cryo-EM structure of PGE2-EP1-Gq complex | | Descriptor: | (Z)-7-[(1R,2R,3R)-3-hydroxy-2-[(E,3S)-3-hydroxyoct-1-enyl]-5-oxo-cyclopentyl]hept-5-enoic acid, Guanine nucleotide-binding protein G(I)/G(S)/G(O) subunit gamma-2, Guanine nucleotide-binding protein G(I)/G(S)/G(T) subunit beta-1, ... | | Authors: | Meng, X, Xu, Y, Xu, H.E. | | Deposit date: | 2025-02-26 | | Release date: | 2025-04-30 | | Method: | ELECTRON MICROSCOPY (2.55 Å) | | Cite: | Structural Insights into the Activation of Human Prostaglandin E2 Receptor EP1 Subtype by Prostaglandin E2
To Be Published
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9LRC
 | | Cryo-EM structure of the histamine H4 receptor-Gi protein complex (Receptor focused) | | Descriptor: | HISTAMINE, Histamine H4 receptor,Genome polyprotein | | Authors: | Matsuzaki, Y, Sano, F.K, Oshima, H.S, Akasaka, H, Kobayashi, K, Tanaka, T, Itoh, Y, Shihoya, W, Kise, Y, Kusakizako, T, Nureki, O. | | Deposit date: | 2025-01-30 | | Release date: | 2025-06-11 | | Method: | ELECTRON MICROSCOPY (2.84 Å) | | Cite: | Structural insights into ligand recognition and G protein preferences across histamine receptors
To Be Published
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6TKO
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6TPN
 | | Crystal structure of the Orexin-2 receptor in complex with HTL6641 at 2.61 A resolution | | Descriptor: | 2-(5,6-dimethoxypyridin-3-yl)-1,1-bis(oxidanylidene)-4-[[2,4,6-tris(fluoranyl)phenyl]methyl]pyrido[2,3-e][1,2,4]thiadiazin-3-one, NITRATE ION, OLEIC ACID, ... | | Authors: | Rappas, M, Ali, A, Bennett, K.A, Brown, J.D, Bucknell, S.J, Congreve, M, Cooke, R.M, Cseke, G, de Graaf, C, Dore, A.S, Errey, J.C, Jazayeri, A, Marshall, F.H, Mason, J.S, Mould, R, Patel, J.C, Tehan, B.G, Weir, M, Christopher, J.A. | | Deposit date: | 2019-12-13 | | Release date: | 2020-01-01 | | Last modified: | 2024-01-24 | | Method: | X-RAY DIFFRACTION (2.608 Å) | | Cite: | Comparison of Orexin 1 and Orexin 2 Ligand Binding Modes Using X-ray Crystallography and Computational Analysis.
J.Med.Chem., 63, 2020
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6TPJ
 | | Crystal structure of the Orexin-2 receptor in complex with suvorexant at 2.76 A resolution | | Descriptor: | AMMONIUM ION, OLEIC ACID, Orexin receptor type 2,GlgA glycogen synthase,Hypocretin receptor-2, ... | | Authors: | Rappas, M, Ali, A, Bennett, K.A, Brown, J.D, Bucknell, S.J, Congreve, M, Cooke, R.M, Cseke, G, de Graaf, C, Dore, A.S, Errey, J.C, Jazayeri, A, Marshall, F.H, Mason, J.S, Mould, R, Patel, J.C, Tehan, B.G, Weir, M, Christopher, J.A. | | Deposit date: | 2019-12-13 | | Release date: | 2020-01-01 | | Last modified: | 2024-01-24 | | Method: | X-RAY DIFFRACTION (2.74 Å) | | Cite: | Comparison of Orexin 1 and Orexin 2 Ligand Binding Modes Using X-ray Crystallography and Computational Analysis.
J.Med.Chem., 63, 2020
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6ZDV
 | | Crystal structure of stabilized A2A adenosine receptor A2AR-StaR2-bRIL in complex with Chromone 5d | | Descriptor: | (2R)-2,3-dihydroxypropyl (9Z)-octadec-9-enoate, (2S)-2,3-dihydroxypropyl (9Z)-octadec-9-enoate, Adenosine receptor A2a,Soluble cytochrome b562,Adenosine receptor A2a, ... | | Authors: | Verdon, G, Jespers, W, Azuaje, J, Majellaro, M, Keranen, H, Garcia-mera, X, Congreve, M, Deflorian, F, de Graaf, C, Zhukov, A, Dore, A, Mason, J, Aqvist, J, Cooke, R, Sotelo, E, Gutierrez-de-Teran, H. | | Deposit date: | 2020-06-15 | | Release date: | 2020-09-16 | | Last modified: | 2024-10-23 | | Method: | X-RAY DIFFRACTION (2.13 Å) | | Cite: | X-Ray Crystallography and Free Energy Calculations Reveal the Binding Mechanism of A 2A Adenosine Receptor Antagonists.
Angew.Chem.Int.Ed.Engl., 59, 2020
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6ZFZ
 | | Structure of M1-StaR-T4L in complex with 77-LH-28-1 at 2.17A | | Descriptor: | (2R)-2,3-dihydroxypropyl (9Z)-octadec-9-enoate, 1-[3-(4-butylpiperidin-1-yl)propyl]-3,4-dihydroquinolin-2-one, 4-(2-HYDROXYETHYL)-1-PIPERAZINE ETHANESULFONIC ACID, ... | | Authors: | Rucktooa, P, Cooke, R.M. | | Deposit date: | 2020-06-18 | | Release date: | 2021-10-06 | | Last modified: | 2024-11-13 | | Method: | X-RAY DIFFRACTION (2.17 Å) | | Cite: | From structure to clinic: Design of a muscarinic M1 receptor agonist with potential to treatment of Alzheimer's disease.
Cell, 184, 2021
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6ZG9
 | | Structure of M1-StaR-T4L in complex with GSK1034702 at 2.5A | | Descriptor: | 4-(2-HYDROXYETHYL)-1-PIPERAZINE ETHANESULFONIC ACID, 7-fluoranyl-5-methyl-3-[1-(oxan-4-yl)piperidin-4-yl]-1~{H}-benzimidazol-2-one, Muscarinic acetylcholine receptor M1,Endolysin,Muscarinic acetylcholine receptor M1, ... | | Authors: | Rucktooa, P, Cooke, R.M. | | Deposit date: | 2020-06-18 | | Release date: | 2021-10-06 | | Last modified: | 2024-10-23 | | Method: | X-RAY DIFFRACTION (2.5 Å) | | Cite: | From structure to clinic: Design of a muscarinic M1 receptor agonist with potential to treatment of Alzheimer's disease.
Cell, 184, 2021
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6ZG4
 | | Structure of M1-StaR-T4L in complex with HTL0009936 at 2.35A | | Descriptor: | Muscarinic acetylcholine receptor M1,Endolysin,Muscarinic acetylcholine receptor M1, OLEIC ACID, PHOSPHATE ION, ... | | Authors: | Rucktooa, P, Cooke, R.M. | | Deposit date: | 2020-06-18 | | Release date: | 2021-10-06 | | Last modified: | 2024-10-16 | | Method: | X-RAY DIFFRACTION (2.33 Å) | | Cite: | From structure to clinic: Design of a muscarinic M1 receptor agonist with potential to treatment of Alzheimer's disease.
Cell, 184, 2021
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7ARO
 | | Crystal structure of the non-ribose partial agonist LUF5833 bound to the adenosine A2A receptor | | Descriptor: | 2-azanyl-6-(1~{H}-imidazol-2-ylmethylsulfanyl)-4-phenyl-pyridine-3,5-dicarbonitrile, Adenosine receptor A2a,Soluble cytochrome b562,Adenosine receptor A2a, CHOLESTEROL, ... | | Authors: | Verdon, G, Amelia, T, van Veldhoven, J, Falsini, M, Liu, R, Heitman, L, van Westen, G, Segala, E, Cheng, R, Cooke, R, van der Es, D, Ijzerman, A. | | Deposit date: | 2020-10-25 | | Release date: | 2021-04-07 | | Last modified: | 2024-11-13 | | Method: | X-RAY DIFFRACTION (3.119 Å) | | Cite: | Crystal Structure and Subsequent Ligand Design of a Nonriboside Partial Agonist Bound to the Adenosine A 2A Receptor.
J.Med.Chem., 64, 2021
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7AUE
 | | Melanocortin receptor 4 (MC4R) Gs protein complex | | Descriptor: | AMINOSERINE, CALCIUM ION, Guanine nucleotide-binding protein G(I)/G(S)/G(O) subunit gamma-2, ... | | Authors: | Degtjarik, O, Israeli, H, Prabahar, V, Shalev-Benami, M. | | Deposit date: | 2020-11-02 | | Release date: | 2021-04-28 | | Last modified: | 2023-03-15 | | Method: | ELECTRON MICROSCOPY (2.97 Å) | | Cite: | Structure reveals the activation mechanism of the MC4 receptor to initiate satiation signaling.
Science, 372, 2021
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7BU7
 | | Structure of human beta1 adrenergic receptor bound to BI-167107 and nanobody 6B9 | | Descriptor: | (2S)-2,3-dihydroxypropyl (7Z)-tetradec-7-enoate, 4-(2-HYDROXYETHYL)-1-PIPERAZINE ETHANESULFONIC ACID, 8-[(1R)-2-{[1,1-dimethyl-2-(2-methylphenyl)ethyl]amino}-1-hydroxyethyl]-5-hydroxy-2H-1,4-benzoxazin-3(4H)-one, ... | | Authors: | Xu, X, Kaindl, J, Clark, M, Hubner, H, Hirata, K, Sunahara, R, Gmeiner, P, Kobilka, B.K, Liu, X. | | Deposit date: | 2020-04-04 | | Release date: | 2020-12-02 | | Last modified: | 2024-11-20 | | Method: | X-RAY DIFFRACTION (2.6 Å) | | Cite: | Binding pathway determines norepinephrine selectivity for the human beta 1 AR over beta 2 AR.
Cell Res., 31, 2021
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3NY9
 | | Crystal structure of the human beta2 adrenergic receptor in complex with a novel inverse agonist | | Descriptor: | (2R)-2,3-dihydroxypropyl (9Z)-octadec-9-enoate, Beta-2 adrenergic receptor, Lysozyme, ... | | Authors: | Fenalti, G, Wacker, D, Brown, M.A, Katritch, V, Abagyan, R, Cherezov, V, Stevens, R.C, Accelerated Technologies Center for Gene to 3D Structure (ATCG3D), GPCR Network (GPCR) | | Deposit date: | 2010-07-14 | | Release date: | 2010-08-11 | | Last modified: | 2024-11-06 | | Method: | X-RAY DIFFRACTION (2.84 Å) | | Cite: | Conserved Binding Mode of Human beta(2) Adrenergic Receptor Inverse Agonists and Antagonist Revealed by X-ray Crystallography
J.Am.Chem.Soc., 132, 2010
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3P0G
 | | Structure of a nanobody-stabilized active state of the beta2 adrenoceptor | | Descriptor: | 8-[(1R)-2-{[1,1-dimethyl-2-(2-methylphenyl)ethyl]amino}-1-hydroxyethyl]-5-hydroxy-2H-1,4-benzoxazin-3(4H)-one, Beta-2 adrenergic receptor, Lysozyme, ... | | Authors: | Rasmussen, S.G.F, Choi, H.-J, Fung, J.J, Pardon, E, Casarosa, P, Chae, P.S, DeVree, B.T, Rosenbaum, D.M, Thian, F.S, Kobilka, T.S, Schnapp, A, Konetzki, I, Sunahara, R.K, Gellman, S.H, Pautsch, A, Steyaert, J, Weis, W.I, Kobilka, B.K. | | Deposit date: | 2010-09-28 | | Release date: | 2011-01-19 | | Last modified: | 2024-10-30 | | Method: | X-RAY DIFFRACTION (3.5 Å) | | Cite: | Structure of a nanobody-stabilized active state of the b2 adrenoceptor
Nature, 469, 2011
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3QAK
 | | Agonist bound structure of the human adenosine A2a receptor | | Descriptor: | (2R)-2,3-dihydroxypropyl (9Z)-octadec-9-enoate, 6-(2,2-diphenylethylamino)-9-[(2R,3R,4S,5S)-5-(ethylcarbamoyl)-3,4-dihydroxy-oxolan-2-yl]-N-[2-[(1-pyridin-2-ylpiperidin-4-yl)carbamoylamino]ethyl]purine-2-carboxamide, Adenosine receptor A2a,lysozyme chimera | | Authors: | Xu, F, Wu, H, Katritch, V, Han, G.W, Cherezov, V, Stevens, R, GPCR Network (GPCR) | | Deposit date: | 2011-01-11 | | Release date: | 2011-03-09 | | Last modified: | 2024-10-09 | | Method: | X-RAY DIFFRACTION (2.71 Å) | | Cite: | Structure of an agonist-bound human A2A adenosine receptor.
Science, 332, 2011
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